VAP 20 concentrate 20 µg/ml 1 ml, 10 pcs.

Proteaglandin E₁ drug. It improves microcirculation and peripheral circulation, has angioprotective effect. When administered systemically it causes relaxation of smooth muscle fibers, has a vasodilator effect, decreases ARF, lowers BP.

In this case there is a reflex increase of cardiac output and HR. It improves rheological properties of blood by increasing the elasticity of erythrocytes and reducing platelet aggregation and neutrophil activity, increases blood fibrinolytic activity.

It affects the metabolism, increases the utilization of glucose and oxygen, inhibits the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates protein synthesis, has a beneficial effect on lipid metabolism (inhibiting cholesterol synthesis and reducing LDL concentration), inhibits proliferation of smooth muscle cells.

It has a stimulating effect on the smooth muscles of the intestine, bladder and uterus; it suppresses the secretion of gastric juice.

In intracavernosal administration blocks α₁-adrenoreceptors in penile tissues and causes relaxation effect on smooth muscle of corpora cavernosa, increases blood flow and improves microcirculation.

Dilation of cavernous arteries and vessels of trabecular smooth muscles of cavernous bodies leads to rapid increase of blood inflow and dilatation of lacunar spaces in cavernous bodies. Venous outflow through the vessels located under the proteinous shell is restricted, which stimulates the development of an erection (“corporal veno-occlusive mechanism”). The onset of action is 5-10 minutes, the duration is 1-3 hours.

Indications

The need to temporarily maintain the functioning of the ductus arteriosus until corrective surgery is performed for congenital ductus-dependent heart defects in newborns (including mitral atresia, pulmonary atresia, tricuspid valve atresia, tetralogy of Fallot).

Chronic obliterating diseases of the arteries, stage III-IV (according to Fontaine classification). Obliterating endarteritis with severe intermittent claudication (with impossible surgical revascularization of the lower limb), obliterating atherosclerosis, diabetic angiopathy, thromboangiitis obliterans (Buerger’s disease), Raynaud’s syndrome with trophic disorders, vasculitis, scleroderma, cramps of the calf muscles, the damaging effects of physical factors, especially extreme vibration.

Treatment of erectile dysfunction of neurogenic, vascular, psychogenic or mixed etiology; conducting a pharmacological test as part of a set of diagnostic tests for erectile dysfunction.

Pharmacological effect

Prostaglandin E1 preparation. Improves microcirculation and peripheral circulation, has an angioprotective effect. When administered systemically, it causes relaxation of smooth muscle fibers, has a vasodilating effect, reduces peripheral vascular resistance, and lowers blood pressure.

In this case, there is a reflex increase in cardiac output and heart rate. Improves the rheological properties of blood, helping to increase the elasticity of red blood cells and reducing platelet aggregation and neutrophil activity, increases the fibrinolytic activity of the blood.

It affects metabolism, increases the utilization of glucose and oxygen, suppresses the release of free radicals and lysosomal enzymes from granulocytes and macrophages, stimulates protein synthesis, has a beneficial effect on lipid metabolism (suppressing cholesterol synthesis and reducing LDL concentration), and inhibits the proliferation of smooth muscle cells.

Has a stimulating effect on the smooth muscles of the intestines, bladder, and uterus; suppresses the secretion of gastric juice.

When administered intracavernosally, it blocks α1-adrenergic receptors in the tissues of the penis, has a relaxing effect on the smooth muscles of the cavernous bodies, increases blood flow and improves microcirculation.

Dilation of the cavernous arteries and vessels of the trabecular smooth muscle of the cavernous bodies leads to a rapid increase in blood flow and dilatation of the lacunar spaces in the cavernous bodies. Venous outflow through the vessels located under the tunica albuginea is limited, which stimulates the development of an erection (“corporal veno-occlusive mechanism”). Onset of action is 5-10 minutes, duration is 1-3 hours.

Special instructions

Use IV and IV with caution in acute and subacute myocardial infarction, in myocardial infarction suffered within the last 6 months, in severe or unstable angina, decompensated chronic heart failure, in arterial hypotension, cardiovascular failure, in pulmonary edema, severe arrhythmias, broncho-obstructive syndrome (severe with signs of respiratory insufficiency), with infiltrative changes in the lungs, liver failure (including a history), with an increased risk of bleeding (including with peptic ulcer of the stomach or duodenum, severe damage to cerebral vessels, proliferative retinopathy with a tendency to bleed, extensive trauma), hemodialysis, type 1 diabetes mellitus, especially with extensive vascular lesions (in elderly patients); against the background of the use of vasodilators or anticoagulants; in newborns (risk of developing bradypnea, arterial hypotension, tachycardia or hyperthermia).

Use intracavernosally with caution in case of thrombocytopenia, polycythemia, thrombophlebitis, venous thrombosis (including in case of predisposition), increased blood viscosity, balanitis, urethritis.

Should not be used in patients with a tendency to drug addiction and/or mental or intellectual disorders.

In case of disorders of the blood coagulation system or during simultaneous treatment with drugs that affect the coagulation system, blood coagulation parameters should be regularly monitored during treatment with alprostadil. With systemic administration, monitoring of central hemodynamic parameters and biochemical blood parameters is necessary.

With long-term continuous administration, apnea may develop, a negative effect on the structure of the wall of the ductus arteriosus with an increased risk of rupture, and thinning of the muscular layer of the pulmonary artery. With a treatment duration of more than 4 weeks, reversible cortical proliferation of tubular bones is possible.

In newborns, it should be used under constant blood pressure monitoring, with mandatory conditions for mechanical ventilation.

There is currently no experience with intracavernosal administration to patients under 18 years of age and over 75 years of age.

Alprostadil is not intended for simultaneous use with other drugs for the treatment of erectile dysfunction.

The compliance of the dosage form of alprostadil used with the specific indications for its use should be strictly observed.

Active ingredient

Alprostadil

Composition

Concentrate for the preparation of solution for infusion 1 ml:

Contraindications

Chronic heart failure, pulmonary edema, cardiac arrhythmias, myocardial infarction within the last 6 months; infiltrative changes in the lungs, bronchial asthma; liver dysfunction, liver disease (including history); history of ulcerative lesions of the gastrointestinal tract; hypersensitivity to alprostadil; pregnancy, lactation.

For intracavernous administration: diseases predisposing to the occurrence of priapism (sickle cell anemia, myeloma, leukemia); anatomical deformations of the penis (angulation, cavernous fibrosis, Peyronie’s disease). Do not use in patients with a penile implant, or with contraindications for sexual intercourse.

Side Effects

From the digestive system: diarrhea, nausea, vomiting, increased transaminase activity; rarely – hyperbilirubinemia, peritoneal symptoms.

From the cardiovascular system: arterial hypotension, tachycardia, pain in the heart; rarely – heart failure, heart rhythm disturbances, AV block, acute pulmonary edema.

From the central nervous system and peripheral nervous system: headache, psychosis, convulsions of central origin, paresthesia; rarely – lethargy.

From the respiratory system: rarely – tachypnea, respiratory distress syndrome.

From the hematopoietic system and blood coagulation system: leukocytosis, leukopenia; rarely – bleeding, hypochromic anemia, thrombocytopenia.

From the urinary system: rarely – anuria, renal failure, hematuria.

Metabolic disorders: rarely – hypoglycemia, hypercapnia.

From the musculoskeletal system: joint pain, neck muscle tension, reversible hyperostosis of tubular bones.

Allergic reactions: skin rash, itching.

Other: possible hyperthermia, redness of the skin, increased sweating, swelling of the limb into which the infusion is being administered.

With intracavernous injection, pain in the penis, prolonged erection and priapism are possible; rarely – fibrosis, swelling, feeling of heat, numbness, rashes on the penis, balanitis, hemorrhages, itching and swelling of the injection site, bleeding from the urethra, fungal infection, phimosis, painful erection and impaired ejaculation, pain in the testicles, testicular swelling, pain and tension in the scrotum, increased urination, urinary incontinence, pain in the buttocks, legs, abdomen, pain in the pelvis, lower back, flu-like syndrome, hypoesthesia, myasthenia.

Interaction

With simultaneous use, alprostadil enhances the effect of antihypertensive drugs and vasodilators, anticoagulants, and antiplatelet agents.

Recommendations for use

Individual, depending on the indications and dosage form used.

Functional features

When administered intravenously, alprostadil is rapidly metabolized. With a single passage through the lungs, up to 60-90% is metabolized. Enzymatic oxidation produces 3 biologically active metabolites: 15-keto-PGE1, 15-keto-13,14-dihydro-PGE1 and 13,14-dihydro-PGE1. Keto metabolites have a lower biological effect compared to alprostadil; the 13,14-dihydro-PGE1 metabolite has a comparable effect to PGE1. The pharmacodynamic effect is due mainly to this biologically active metabolite. T1/2 of 13,14-dihydro-PGE1 is about 1 min. The main metabolites are excreted primarily in the urine and, to a lesser extent, in the feces.

With intracavernous administration, the concentration of alprostadil and its main metabolite – 15-oxo-13,14-dihydro-PgE1 – is determined only in the cavernous bodies. After intracavernosal administration of 20 μg of alprostadil, the content of the main metabolite in the peripheral bloodstream increased and reached a maximum 30 minutes after injection, and then returned to the initial level 60 minutes after injection, while the levels of alprostadil in the peripheral bloodstream were slightly higher than baseline. Alprostadil, when entering the systemic circulation during intracavernous administration, is very quickly metabolized. Excreted in the form of metabolites.

Manufacturer

BEG, Germany